Remote C-H Functionalization of 8-Aminoquinoline Ring
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Updated: Dec 18, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Zhihui Xu1, Xiaogang Yang1, Shuang-Feng Yin1
1State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Hunan University, Changsha, 410082, People's Republic of China.
Abstract:
8-Aminoquinoline is a common nitrogen-containing heterocyclic framework in many natural products, functional materials and useful drugs. It has been developed as a powerful bidentate directing group or ligand auxiliary in the field of C-H bond activation/functionalization in recent years. In this context, the synthesis of substituted 8-aminoquinoline is of great importance. In this review we focus on the functionalization of positions C2-C7 on the 8-aminoquinoline ring, which involves the formation of C-C and C-Z (Z = heteroatom) bonds by transition metal catalysts, photocatalysts or metal-free conditions. Mechanistically, a single electron transfer (SET) pathway is suggested in most cases.
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